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Abstract
Background Histamine is a double-protonated molecule with corresponding pKa values of 5.8 and 9.4. Therefore, at physiological pH, histamine exists as an equilibrium mixture of tautomeric cations: the monocation making up 96%, the dication only 3% and the rest being nonprotonated histamine. As a protonated molecule histamine most probably uses a carrier protein in order to cross the cell membrane. In the present work we wanted to determine the kinetic properties of histamine uptake and the influence of other biogenic amines on its transport.
Highlights
Histamine is a double-protonated molecule with corresponding pKa values of 5.8 and 9.4
Histamine uptake in neonatal rat astrocytes is a bidirectional process, which was found to be dependent on pH and Na+, but not Cl−-dependent, with low affinity (Km 116 μM) and high capacity (158 pmol/mg protein)
The uptake was inhibited by millimolar concentrations of other biogenic amines
Summary
Histamine is a double-protonated molecule with corresponding pKa values of 5.8 and 9.4. Low affinity histamine uptake into neonatal rat astrocytes does not involve OCT Vesna Terbuc1, Maša Novak1, Katja Perdan-Pirkmajer1, Sergej Pirkmajer2, Mojca Kržan1* From 18th Scientific Symposium of the Austrian Pharmacological Society (APHAR).
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